[EN] PYRAZOLE PYRIMIDINE DERIVATIVE AND USES THEREOF<br/>[FR] DÉRIVÉ DE PYRAZOLE PYRIMIDINE ET UTILISATIONS DE CELUI-CI
申请人:YISSUM RES DEV CO
公开号:WO2017021969A1
公开(公告)日:2017-02-09
The present invention provides pyrazole pyrimidine derivatives which inhibit Casein kinase I (CKI) and/or lnterleukin-1 receptor-associated kinase 1 (IRAKI) and methods of their manufacture, compositions comprising them and uses thereof in methods of treating malignant disease and disorders and methods for treating inflammatory diseases and disorders.
CHEMOSELECTIVE METHYLENE HYDROXYLATION IN AROMATIC MOLECULES
申请人:The Board of Trustees of the University of Illinois
公开号:US20200087331A1
公开(公告)日:2020-03-19
A chemoselective and reactive Mn(CF
3
-PDP) catalyst system that enables for the first time the strategic advantages of late-stage aliphatic C—H hydroxylation to be leveraged in aromatic compounds. This discovery will benefit small molecule therapeutics by enabling the rapid diversification of aromatic drugs and natural products and identification of their metabolites.
Pharmacologically active phenylalkanoyl substituted imidazo (4,5-C)
申请人:G. D. Searle & Co.
公开号:US04988707A1
公开(公告)日:1991-01-29
This invention relates to substituted imidazopyridine dervatives having the following formula ##STR1## and isomers thereof; or a pharmaceutically acceptable acid addition salt thereof: wherein R.sub.1 and R.sub.2 are each independently selected from hydrogen; straight or branched chain alkyl of 1 to 15 carbon atoms; cycloalkyl of 3 to 8 carbon atoms; cycloalkyl which can be substituted once or more by alkyl of 1 to 6 carbon atoms; phenyl; phenyl which can be substituted once or more by alkyl of 1 to 6 carbon atoms or halogen; straight or branched alkenyl having 3 to 15 carbon atoms. y is phenyl or phenyl substituted once or more by alkyl of 1 to 6 carbon atoms; alkoxy wherein the alkyl is 1 to 6 carbon atoms; and halogen selected from the group consisting of bromo, fluoro or chloro. m is an integer from 0 to 5. n is an integer from 1 to 5. R.sub.3 is a group substituted at one or more of the 4, 6 or 7 positions of the pyridine ring said groups being independently selected from hydrogen, alkyl of 1 to 6 carbon atoms; halogen wherein the halogen is selected from bromo, fluoro, or chloro; or alkoxy wherein the alkyl is 1 to 6 carbon atoms; R.sub.4 is hydrogen or alkyl of 1 to 4 carbon atoms. useful in the treatment of diseases or disorders mediated by platelet-activating factor. This invention also relates to pharmaceutical compositions of such substituted imidazopyridines.
[EN] PYRROLIDINE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY<br/>[FR] MODULATEURS DE PYRROLIDINE DE L'ACTIVITE DU RECEPTEUR DES CHIMIOKINES
申请人:MERCK & CO INC
公开号:WO2000059498A1
公开(公告)日:2000-10-12
The present invention is directed to pyrrolidine compounds of the formula (I) (wherein R?1, R2, R3, R4, R5, R6¿ and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.
[EN] PYRROLIDINE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY<br/>[FR] PYRROLIDINES MODULATEURS DE L'ACTIVITE DU RECEPTEUR DE CHIMIOKINE
申请人:MERCK & CO INC
公开号:WO2000059502A1
公开(公告)日:2000-10-12
The present invention is directed to pyrrolidine compounds of formula (I) (wherein R?1, R2, R3, R4, R5, R6, R14¿ and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.